2-(2-Hydroxyethylamino)-6-benzylamino-9-methylpurine White solid. A purine derivative that acts as a potent and selective inhibitor of p34cdk1/cyclin B (IC50 = 7 µM) and related kinases including p33cdk2/cyclin A (IC50 = 7 µM), p33cdk2/cyclin E (IC50 = 7 µM), p33cdk5/p35 (IC50 = 3 µM), and p44 MAP kinase (IC50 = 25 µM). Acts by competing for the ATP binding domain of the kinase. Exhibits reduced sensitivity towards related kinases, p34cdk4/cyclin D (IC50 > 1 mM), and p40cdk6/cyclin D3 (IC50 > 250 µM). Does not significantly affect the activity of other protein kinases at 1 mM. Known to inhibit DNA synthesis in interleukin-2-stimulated T lymphocytes and trigger G1 arrest similar to that observed in interleukin-2-deprived cells. Also used to synchronize cells in G1. Purity: ≥98% by TLC. CAS 101622-51-9. Ref.: Abraham, R.T., et al. 1995. Biol. Cell 83, 105. Mistelli, T., and Warren, G. 1995. J. Cell Sci. 108, 2715. Glab, N., et al. 1994. FEBS Lett. 353, 207. Veselý, J., et al. 1994. Eur. J. Biochem. 224, 771. |
